AR074688A1 - Derivados de piridazinona, procedimiento para prepararlos, medicamentos que los contienen y uso de los mismos para el tratamiento de tumores. - Google Patents

Derivados de piridazinona, procedimiento para prepararlos, medicamentos que los contienen y uso de los mismos para el tratamiento de tumores.

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Publication number
AR074688A1
AR074688A1 ARP090104911A ARP090104911A AR074688A1 AR 074688 A1 AR074688 A1 AR 074688A1 AR P090104911 A ARP090104911 A AR P090104911A AR P090104911 A ARP090104911 A AR P090104911A AR 074688 A1 AR074688 A1 AR 074688A1
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AR
Argentina
Prior art keywords
piperidin
nhet
nhet1
hal
nor2
Prior art date
Application number
ARP090104911A
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English (en)
Inventor
Dieter Dorsch
Andree Blaukat
Frank Stieber
Oliver Schadt
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Merck Patent Gmbh
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Publication date
Application filed by Merck Patent Gmbh filed Critical Merck Patent Gmbh
Publication of AR074688A1 publication Critical patent/AR074688A1/es

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    • C—CHEMISTRY; METALLURGY
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    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/14—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
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    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61K47/02—Inorganic compounds
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    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/0012—Galenical forms characterised by the site of application
    • A61K9/0014—Skin, i.e. galenical aspects of topical compositions
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    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/0012—Galenical forms characterised by the site of application
    • A61K9/0019—Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner
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    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
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    • A61K9/0048—Eye, e.g. artificial tears
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    • A61K9/02—Suppositories; Bougies; Bases therefor; Ovules
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    • A61K9/06—Ointments; Bases therefor; Other semi-solid forms, e.g. creams, sticks, gels
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    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/20—Pills, tablets, discs, rods
    • A61K9/2004—Excipients; Inactive ingredients
    • A61K9/2013—Organic compounds, e.g. phospholipids, fats
    • A61K9/2018—Sugars, or sugar alcohols, e.g. lactose, mannitol; Derivatives thereof, e.g. polysorbates
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A61P17/02—Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
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    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
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    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
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    • A61P35/00—Antineoplastic agents
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A61P35/02—Antineoplastic agents specific for leukemia
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    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
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    • A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
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    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/08—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a carbon chain containing alicyclic rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/10—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a carbon chain containing aromatic rings
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    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D453/00—Heterocyclic compounds containing quinuclidine or iso-quinuclidine ring systems, e.g. quinine alkaloids
    • C07D453/02—Heterocyclic compounds containing quinuclidine or iso-quinuclidine ring systems, e.g. quinine alkaloids containing not further condensed quinuclidine ring systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/14—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
    • A61K9/19—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles lyophilised, i.e. freeze-dried, solutions or dispersions
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    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/20—Pills, tablets, discs, rods
    • A61K9/28—Dragees; Coated pills or tablets, e.g. with film or compression coating
    • A61K9/2806—Coating materials
    • A61K9/282—Organic compounds, e.g. fats
    • A61K9/2826—Sugars or sugar alcohols, e.g. sucrose; Derivatives thereof

Abstract

Los compuestos de la fórmula (1) en donde R1 es Ar, Het, A, OR2, O[C(R2)2]nAr, O[C(R2)2]nHet, N(R2)2, NR2[C(R2)2]nAr o NR2[C(R2)2]nHet; R2 es H o A'; R3, R3' son, en cada caso de modo independiente entre sí, H, Hal, A, OR2, CN, COOR2, CON(R2)2, NR2COA, NR2SO2A, SO2N(R2)2 o S(O)mA, Y es [C(R2)2]nNR2COZ, [C(R2)2]nNR2COHet1, [C(R2)2]nCyc[C(R2)2]nN(R2)2, [C(R2)2]nCyc[C(R2)2]nOR2, [C(R2)2]nCyc[C(R2)2]nHet1, [C(R2)2]n-C(CH2)-((CH2)p)-[C(R2)2]nN(R2)2, [C(R2)2]n-C(CH2-(CH2)p)[C(R2)2]nOR2, [C(R2)2]n-C(CH2-(CH2)p)-[C(R2)2]nHet, [C(R2)2]nHet2, [C(R2)2]nCR2(NR2)2COOR2, [C(R2)2]nNR2CO[C(R2)2]nNR2COA, [C(R2)2]nNR2COOA, [C(R2)2]nCO-NR2-A, [C(R2)2]nCO-NR2-[C(R2)2]nHet1, [C(R2)2]nCONH2, [C(R2)2]nCONHA, [C(R2)2]nCONA2, [C(R2)2]nCO-NR2-[C(R2)2]nN(R2)2 o COOA; ; Z es CR2(NR2)2CR2(OR2)A, Ar es fenilo, naftilo o bifenilo no sustituido o mono-, di- o trisustituido con Hal, A, [C(R2)2]nOR2, [C(R2)2]nN(R2)2, SR2, NO2, CN, CO-OR2, CON(R2)2, NR2COA, NR2SO2A, SO2N(R2)2, S(O)mA, CO-Het, Het, O[C(R2)2]nN(R2)2, O[C(R2)2]nHet, NHCOOA, NHCON(R2)2, NHCOO[C(R2)2]nN(R2)2, NHCOO[C(R2)2]nHet, NHCONH[C(R2)2]nN(R2)2, NHCONH[C(R2)2]nHet, OCONH[C(R2)2]nN(R2)2, OCONH[C(R2)2]nHet, CONR2[C(R2)2]nN(R2)2, CONR2[C(R2)2]nHet, y/o COA, Het es un heterociclo mono-, bi- o tricíclico saturado, insaturado o aromático con 1 a 4 átomos de N, O y/o S, que puede no estar sustituido o que puede estar mono-, di- o trisustituido con Hal, A, [C(R2)2]nOR2, [C(R2)2]n(R2)2, SR2, NO2, CN, COOR2, CON(R2)2, NR2COA, NR2SO2A, SO2N(R2)2, S(O)mA, CO-Het1, [C(R2)2]nHet1, O[C(R2)2]nN(R2)2, O[C(R2)2]nHet1, NHCOOA, NHCON(R2)2, NHCOO[C(R2)2]nN(R2)2, NHCOO[C(R2)2]nHet1, NHCONH[C(R2)2]nN(R2)2, NHCONH[C(R2)2]nHet1, OCONH[C(R2)2]nN(R2)2, OCONH[C(R2)2]nHet1, CO-Het1, CHO, COA, =S, =NH, =NA y/u =O (oxígeno del carbonilo), Het1 es un heterociclo saturado monocíclico con 1 a 2 átomos de N y/u O, que puede estar mono- o disustituido con A, OA, OH, COOH, COOA, Hal y/u =O (oxígeno del carbonilo), Het2 es 2-metoxicarbonil-pirrolidin-4-ilo, 2-carboxi-pirrolidin-4-ilo, 1-ciclopropilmetil-piperidin-4-ilo, piperidin-4-ilo, morfolin-2-o 4-ilo, 1-isopropil-piperidin-4-ilo, 1-metil-piperidin-4-ilo, 4-piperazinilo, 1-metil-pirrolidin-2-ilo, 1-ter.-butoxicarbonil-piperidin-4-ilo, 1-etil-piperidin-2-ilo, 1-(2-metoxi-etil)-piperidin-4-ilo, 1-[2-(N,N-dimetilamino)-etil]-piperidin-4-ilo, 1,2,2,6,6-pentametil-piperidin-4-ilo, 1-aza-biciclo[2,2,2]oct-3-ilo, tetrahidropiran-4-ilo, 1-formil-piperidin-4-ilo o 1-metil-1-oxi-piperidin-4-ilo, A es alquilo no ramificado o ramificado C1-10, en donde 1-7 átomos de H pueden estar reemplazados por F, y/o en donde uno o dos grupos CH2 no adyacentes pueden estar reemplazados por O, NH, S, SO, SO2 y/o grupos CH=CH, o es alquilo cíclico C3-7, A' es alquilo no ramificado o ramificado C1-6 en donde 1-5 átomos de H pueden estar reemplazados por F; CyC es cicloalquileno C3-7; Hal es F, Cl, Br o I; m es 0, 1 o 2, n es 1, 2, 3 o 4, p es 1, 2, 3, 4, o 5; así como sus sales, tautómeros y estereoisómeros farmacéuticamente aceptables, incluyendo sus mezclas en todas las proporciones. Son inhibidores de las tirosina quinasas, en especial de la Met-quinasa, y pueden utilizarse, por ejemplo, para el tratamiento de tumores.
ARP090104911A 2008-12-23 2009-12-16 Derivados de piridazinona, procedimiento para prepararlos, medicamentos que los contienen y uso de los mismos para el tratamiento de tumores. AR074688A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
DE102008062826A DE102008062826A1 (de) 2008-12-23 2008-12-23 Pyridazinonderivate

Publications (1)

Publication Number Publication Date
AR074688A1 true AR074688A1 (es) 2011-02-02

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ARP090104911A AR074688A1 (es) 2008-12-23 2009-12-16 Derivados de piridazinona, procedimiento para prepararlos, medicamentos que los contienen y uso de los mismos para el tratamiento de tumores.

Country Status (22)

Country Link
US (1) US8637518B2 (es)
EP (1) EP2367815B1 (es)
JP (1) JP5592395B2 (es)
KR (1) KR20110098854A (es)
CN (1) CN102264727B (es)
AR (1) AR074688A1 (es)
AU (1) AU2009331991B2 (es)
BR (1) BRPI0923497A2 (es)
CA (1) CA2747863C (es)
CY (1) CY1116191T1 (es)
DE (1) DE102008062826A1 (es)
DK (1) DK2367815T3 (es)
EA (1) EA201100966A1 (es)
ES (1) ES2532139T3 (es)
HR (1) HRP20150375T1 (es)
HU (1) HUE025138T2 (es)
MX (1) MX2011006652A (es)
PL (1) PL2367815T3 (es)
PT (1) PT2367815E (es)
SI (1) SI2367815T1 (es)
WO (1) WO2010072296A1 (es)
ZA (1) ZA201105440B (es)

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US20110257181A1 (en) 2011-10-20
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HUE025138T2 (en) 2016-03-29
JP2012513418A (ja) 2012-06-14
JP5592395B2 (ja) 2014-09-17
SI2367815T1 (sl) 2015-05-29
KR20110098854A (ko) 2011-09-01
CA2747863C (en) 2016-08-23
AU2009331991B2 (en) 2015-10-22
ZA201105440B (en) 2012-03-28
CN102264727B (zh) 2014-11-05
EP2367815A1 (de) 2011-09-28
PT2367815E (pt) 2015-02-20
PL2367815T3 (pl) 2015-04-30
DK2367815T3 (en) 2015-03-09
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WO2010072296A1 (de) 2010-07-01
AU2009331991A1 (en) 2011-08-11
EP2367815B1 (de) 2015-01-14
CA2747863A1 (en) 2010-07-01
EA201100966A1 (ru) 2012-01-30
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US8637518B2 (en) 2014-01-28
HRP20150375T1 (hr) 2015-05-22
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